PHA-793887

Description: PHA-793887 is a novel, potent and ATP-competitive inhibitor of the cyclin dependent kinases CDK2, CDK5 and CDK7 with IC50 of 8 nM, 5 nM and 10 nM. It is 6-fold more selective for CDK2, 5, and 7 than CDK1, 4, and 9. PHA-793887 has low activity against CDK1, CDK4, CDK9 and GSK3beta with IC50 of 60 nM, 62 nM, 138 nM and 79 nM, respectively. PHA-793887 inhibits cell proliferation of many tumor cell lines, including A2780, HCT-116, COLO-205, C-433, DU-145, A375, PC3, MCF-7, and BX-PC3, with IC50 of 88 nM–3.4 uM. PHA-793887 (1 uM) shows a decrease in the S phase, a subsequent increase of the G1 phase and a slight accumulation of G2/M phase in A2780 cells.

References: Bioorg Med Chem. 2010 Mar 1; 18(5):1844-53; Exp Hematol. 2010 Apr; 38(4):259-269.e2.

Related CAS#: 718630-60-5 ( HCl salt); 718630-59-2 (free base)